KR20040060156A - Cosmetic Composition for Skin-Whitening Comprising Ramulus Mori Extracts and Niacinamide as Active Ingredients - Google Patents

Abstract

PURPOSE: Provided is a skin whitening cosmetic composition which contains Ramulus mori extract and niacinamide as active ingredients. The cosmetic composition inhibits tyrosinase activity, melanin formation, conversion of niacinamide to melanosome, therefore, it gives excellent skin whitening effect. CONSTITUTION: A skin whitening cosmetic composition is characterized by containing, based on the total weight of the composition, 0.5-10.0 wt.% of Ramulus mori extract and 0.5-10.0 wt.% of niacinamide as active ingredients. It is formulated into liquid, suspension, paste, gel, cream, lotion, powder, soap, surfactant-containing cleansing, oil, foundation and spray.

Description

Cosmetic composition for skin whitening including upper limb extract and niacinamide {Cosmetic Composition for Skin-Whitening Comprising Ramulus Mori Extracts and Niacinamide as Active Ingredients}

The present invention relates to a cosmetic composition, and more particularly, the present invention relates to a cosmetic composition for skin whitening comprising Ramulus mori extract and niacinamide.

Human skin color is largely determined by melanin, hemoglobin, carotene and the like, the most important of which is melanin. Melanin not only determines human skin color, but also acts as a free radical scavenger and skin protection against UV rays. However, when the skin is overexposed to ultraviolet rays or excessively produced melanin due to external environmental changes such as air pollution and stress, pigmentation occurs in the skin, resulting in blackening of the skin color, blemishes, and freckles.

In the process of synthesizing melanin, first, an enzyme called tyrosinase generates dopaquinone through dopa (DOPA), using tyrosine in the cell as a substrate, and dopachrome (DOPAchrome) by auto oxidation and enzyme reaction from dopaquinone. ) To produce the copolymer melanin. The melanin thus produced is transferred to keratinocytes through a endoplasmic reticulum called melanosome, which, after about 28 days of keratinization, exits the skin surface and disappears with the keratin. However, in this process, if the melanin is excessively produced by a factor that promotes melanin production and melanin is not completely eliminated by keratinization, pigmentation occurs. Therefore, in order to prevent such pigmentation phenomenon, it is necessary to control the part of melanin production to reduce melanin production.

There are several mechanisms that inhibit the synthesis of melanin. First, a representative method is to inhibit the activity of tyrosinase, an important enzyme of melanin synthesis, and most commonly known is a chelator such as kojic acid, which inhibits the activity of tyrosinase by chelating copper ions necessary for enzyme activity. have. In addition, as plant extracts that inhibit tyrosinase activity, lettuce extract, licorice extract and the like are known. On the other hand, there is a method for reducing melanin synthesis using a substrate-like substance, a competitive inhibitor of tyrosine, a substrate of tyrosinase, and arbutin, gamma-pyrone, and hinokitol are known as such substrate-like substances.

However, these whitening ingredients have low stability and do not last long, and their use is limited because they are highly irritating to the skin, and plant extracts have the disadvantage of showing a relatively high effect only at high concentrations. Very limited.

The present inventors have made diligent efforts to improve the problems shown in the conventional whitening agent, the cosmetic composition comprising niacinamide inhibiting the movement of the upper limb extract and the synthesized melanin inhibits melanin production by the inhibitory effect of tyrosinase activity of the upper limb extract The present invention has been completed by discovering an excellent whitening effect due to the synergistic effect of the melanin migration inhibitory effect of niacinamide.

Therefore, the object of the present invention is whitening Effect For enhanced skin whitening Cosmetics Composition Provided place have.

Other objects and advantages of the invention will be apparent from the following examples and claims.

According to one aspect of the invention, the present invention provides a cosmetic composition for skin whitening comprising the upper limb extract and niacinamide as an active ingredient.

The present inventors screened a large number of substances in an effort to improve the problems appearing in the conventional whitening agent, and as a result, niacin inhibiting the movement of the upper limb extract and the synthesized melanin having melanin production inhibitory effect due to the superior tyrosinase activity inhibitory effect Cosmetic compositions comprising amides have been found to exhibit excellent whitening effects due to the synergistic action of the activity of the two components.

Ramulus mori extract, which is used as an active ingredient in the composition of the present invention, exhibits an excellent inhibitory effect on tyrosinase activity and has excellent melanin synthesis inhibitory effect, and according to the inventors' patent (Korean Patent No. 230130) The whitening effect has been proven.

In addition, niacinamide used as an active ingredient in the composition of the present invention is known as an effective substance for skin whitening by inhibiting the migration of the synthesized melanin. The niacinamide not only inhibits the tyrosinase enzyme reaction, but also inhibits the mechanism of melanin migration from melanocytes to keratinocytes, thereby reducing skin pigmentation.

More specifically, the niacinamide is a physiologically active amide of vitamin B ₃ , also known as nicotinamide and pyridine-3-carboxylic acid, and serves as an anti-inflammatory raw material or an antioxidant. In addition, niacinamide can be effectively used for skin whitening by reducing skin pigmentation by increasing collagen synthesis and synthesis of intercellular lipids, as well as inhibiting melanocyte migration from melanocytes to keratinocytes.

The present inventors have found that the cosmetic composition containing the upper limb extract and niacinamide at the same time significantly increases the skin whitening effect due to the synergic action of each of the two active ingredients.

The "upper limb extract" used as an active ingredient in the composition of the present invention collectively refers to a material extracted from the upper limbs which are the young branches of mulberry.

The upper extremity extract may be prepared using a variety of extraction solvents such as (a) water, (b) anhydrous or hydrous lower alcohols having 1 to 4 carbon atoms (methanol, ethanol, propanol, butanol, etc.), (c) the lower alcohols and water Mixed solvent of (d) acetone, (e) ethyl acetate, (f) chloroform, (g) 1,3-butylene glycol, and (h) butyl acetate as the extraction solvent. More preferably, the extract of the present invention is obtained using a hydrous lower alcohol, most preferably ethanol. On the other hand, it will be apparent to those skilled in the art that the extract of the present invention can be obtained extracts having substantially the same effect using not only the above-described extraction solvent but also other extraction solvents.

In addition, the extract of the present invention includes not only the extract by the above-described extraction solvent, but also the extract that has undergone a conventional purification process. Obtained by various additional purification methods, such as, for example, separation using an ultrafiltration membrane having a constant molecular weight cut-off value, separation by various chromatography (manufactured for separation according to size, charge, hydrophobicity or affinity). The active fraction is also included in the extract of the present invention.

Also included in the range of "upper limb extracts" is "Melbourne" and other processed products of the upper limbs extracted and processed from the upper limbs. Extracts of the present invention may be prepared in powder form by additional processes such as distillation under reduced pressure and freeze drying or spray drying.

According to a preferred embodiment of the present invention, the content of the upper limb extract and niacinamide in the cosmetic composition of the present invention is 0.5-10.0% by weight, respectively, based on the total weight of the composition. If the content is less than 0.5% by weight, there is a problem in that the whitening effect of the product is weak, when it exceeds 10.0% by weight it is difficult to secure the stability of the formulation may cause skin irritation.

Ingredients included in the cosmetic composition of the present invention include ingredients commonly used in cosmetic compositions in addition to the upper limb extract and niacinamide as active ingredients, and include, for example, conventional agents such as antioxidants, stabilizers, solubilizers, vitamins, pigments and flavorings. Adjuvants, and carriers.

The whitening composition of the present invention may be prepared in any formulation conventionally prepared in the art, for example, solutions, suspensions, emulsions, pastes, gels, creams, lotions, powders, soaps, surfactant-containing It may be formulated as cleansing, oil, powder foundation, emulsion foundation, wax foundation, spray, and the like, but is not limited thereto. More specifically, it may be prepared in the form of a flexible lotion, astringent lotion, nutrition lotion, nutrition cream, massage cream, essence, eye cream, cleansing cream, cleansing foam, cleansing water, pack, spray or powder.

When the formulation of the present invention is a paste, cream or gel, animal oils, vegetable oils, waxes, paraffins, starches, trachants, cellulose derivatives, polyethylene glycols, silicones, bentonites, silicas, talc or zinc oxide may be used as carrier components. Can be.

When the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used, in particular in the case of a spray, additionally chlorofluorohydrocarbon, propane Propellant such as butane or dimethyl ether.

When the formulation of the present invention is a solution or emulsion, a solvent, solubilizer or emulsifier is used as the carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1 Fatty acid esters of, 3-butylglycol oil, glycerol aliphatic ester, polyethylene glycol or sorbitan.

When the formulation of the present invention is a suspension, liquid carrier diluents such as water, ethanol or propylene glycol, suspending agents such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, microcrystals Soluble cellulose, aluminum metahydroxy, bentonite, agar or tracant and the like can be used.

When the formulation of the present invention is a surfactant-containing cleansing, the carrier component is an aliphatic alcohol sulfate, an aliphatic alcohol ether sulfate, a sulfosuccinic acid monoester, isethionate, an imidazolinium derivative, a methyltaurate, a sarcosinate, a fatty acid amide. Ether sulfates, alkylamidobetaines, aliphatic alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, lanolin derivatives or ethoxylated glycerol fatty acid esters and the like can be used.

Hereinafter, the present invention will be described in more detail with reference to Examples. These examples are only for illustrating the present invention in more detail, and the scope of the present invention is not limited by these examples in accordance with the gist of the present invention to those skilled in the art. Will be self-evident.

Example

Example material

The upper limb of the present invention was purchased from Bioland (Bioland, Korea) and used for extract preparation.

In addition, niacinamide of the present invention was purchased from Roche (Switzerland) and used (melting point: 128-132 ° C., moisture content: 0.5%, white crystalline powder).

Example 1: Preparation of Upper Limb Extract

After washing with purified water, 1 kg of dried upper liquor was placed in 5 L of 70% ethanol, extracted at 4-40 ° C. for 5 days, filtered through 300 mesh filter cloth, left at 5-10 ° C. for 7-10 days, and aged. Filtered. This extract was dried on a rotary vacuum evaporator at 60-70 ° C. to obtain upper limb powder.

Example 2 Experiment of Melanosome Migration Inhibition Effect of Niacinamide

Keratinocytes and melanocytes were isolated from the foreskin of newborns, respectively (Eisinger et al., Selective proliferation of normal human melanocytes invitro in presence of phorbol ester and cholea toxin.Proc . Natl. Acad. Sci , 79: 2018-2022 ( 1982). The epidermis was isolated from the foreskin tissue by treatment with 0.25% trypsin, followed by 7.5 mg / ml bovine pituitary extract, 0.1 mg / ml human epidermal growth factor (hEGF), 0.5 mg / ml hydrocortisone, 50 mg / ml Cells were isolated by vortexing with KGM (Clonetics) medium containing gentamicine, 50 mg / ml amphotericin and 5 mg / ml insulin, incubated in T75 flasks and incubated with keratinocytes. Melanosite was obtained respectively. At this time, the cultured melanocytes were stained with carboxy fluorescein diacetate (CFDA) to analyze the melanosomes.

For experiments, keratinocytes and melanocytes were co-cultured in coculture medium (KGM + (KGM-TPA-hydrocortisone)) (Romero-Graillet et al., Nitric oxide produced by ultraviolet-irradiated keratinocytes stimulates melanogenesis, J Clin Invest . 99 (4): 635-42 (1997).

Some of the cells co-cultured at 12 hour intervals for 6 days were then added with the following concentrations of niacinamide and / or upper limb extract, respectively: (A) 0.5 mmol / L upper extremity extract and 0.5 mmol / L niacinamide. ; (B) 1 mmol / L upper extremity extract; (C) Niacinamide 1 mmol / L. The cells to which A to C were added were incubated with a mouse monoclonal antibody against anticytokeratin (Zymed Laboratories, USA) to separate keratinocytes from fluorescence activated cell sorting (FACS), followed by phycoerythrin Bound anti mouse IgG (Burlingame, United States) and the cultured cells were reacted for 30 minutes at 37 ℃. Cells cultured using a scraper were then removed from the flasks and subjected to FACS analysis using EPICSXL flow cytometer (Coulter Cytometry, Coulter Corp., USA). In FACS analysis, keratinocytes in response to phycoerythrin at 575 nm were analyzed, and melanosomes of keratinocytes were confirmed by measuring CFDA at 525 nm. The results obtained in the coculture were analyzed using Coulter XL software (Coulter Corp.). Melanosome migration inhibition rate was calculated by the following equation (1).

The results of this experiment are shown in Table 1 below.

A B C D Upper limb extract (mmol / L) 0.5 One - - Niacinamide (mmol / L) 0.5 - One - Neon 15.51 20.37 12.87 20.50 Inhibition of movement (%) 24.3 0.6 37.2 0.2

As shown in Table 1, the addition of the upper limb extract and niacinamide at the same time, and the addition of niacinamide only C is inhibited the movement of melanosomes compared to B added only the upper limb extract and D without adding the two substances at all. The effect was very good. In addition, the A, although the content of the niacinamide is relatively low at half the level of niacinamide alone added C, the effect of inhibiting the movement of the melanosomes appeared to be significantly superior. Therefore, it can be seen that the composition including the upper limb extract and niacinamide of the present invention is very excellent in inhibiting the movement of melanosomes.

Example 3: Experiment of Tyrosinase Activity Inhibitory Effect

Tyrosinase was isolated and purified from mushrooms and purchased from Sigma. Tyrosine, a substrate, was dissolved in 0.05 M sodium phosphate buffer (pH 6.8) and used as a 0.1 mg / ml solution.

0.5 ml of the substrate tyrosine solution was placed in a test tube, to which niacinamide and / or upper extremity extracts of the following concentrations were added, respectively: (A) 0.5 mmol / L upper extremity extract and 0.5 mmol / L niacinamide; (B) 1 mmol / L upper extremity extract; (C) Niacinamide 1 mmol / L. Then, the mixture was allowed to stand in a 37 ° C constant temperature water bath for 10 minutes, and 0.5 mL of 250 U / mL tyrosinase solution was added thereto, followed by reaction for 10 minutes in a 37 ° C constant temperature water bath. In this case, 0.5 ml of buffer solution was added instead of the sample solution. The test tube containing the reaction solution was placed on ice and quenched to stop the reaction, and then absorbance at 475 nm was measured with a spectrophotometer. Inhibition of tyrosinase activity was calculated by the following equation (2).

The results of the experiment are shown in Table 2 below.

A B C D Upper limb extract (mmol / L) 0.5 One - - Niacinamide (mmol / L) 0.5 - One - Enzyme Inhibition Degree (%) 18.3 23.0 3.2 0.5

As shown in Table 2, A which added the upper limb extract and niacinamide at the same time, and B added only the upper limb extract, inhibited tyrosinase activity as compared to C added with niacinamide only and D without adding the two substances at all. The effect was very good. In addition, the A, although the content of the upper limb extract is relatively lower than the level of the upper limb extract B by only half added, the effect of inhibiting the activity of tyrosinase appeared to be quite excellent at a similar level. Therefore, it can be seen that the composition comprising the niacinamide and the upper limb extract of the present invention is very excellent in tyrosinase activity inhibitory effect.

Example 4: Preparation of Nutritional Cream

The nutrition cream of the preparation example and the comparative cream of the Preparation Example of the present invention was prepared with the composition of Table 3. First, the aqueous components of the raw materials 14 to 18 were completely dissolved by heating to 70-80 ° C., and then the raw materials 1 to 13 were heated to 80-85 ° C., and added to the solution of the raw materials 14 to 18 at a homomixer at 3000 rpm. Emulsification for 10 minutes. Then, the raw material 19 was added, re-emulsified for 3 minutes, and cooled to room temperature.

number ingredient Production Example Comparative Example 1 Comparative Example 2 Comparative Example 3 One Upper limb extract 2.5 5.0 - - 2 Niacinamide 2.5 - 5.0 - 3 Lipophilic monostearate 2.0 2.0 2.0 2.0 4 Cetearyl Alcohol 2.2 2.2 2.2 2.2 5 Stearic acid 1.5 1.5 1.5 1.5 6 Beeswax 1.0 1.0 1.0 1.0 7 Polysorbate 60 1.5 1.5 1.5 1.5 8 Sorbitan stearate 0.6 0.6 0.6 0.6 9 Cured Vegetable Oil 1.0 1.0 1.0 1.0 10 Squalane 3.0 3.0 3.0 3.0 11 Mineral oil 5.0 5.0 5.0 5.0 12 Trioctanoine 5.0 5.0 5.0 5.0 13 Dimethicone 1.0 1.0 1.0 1.0 14 glycerin 5.0 5.0 5.0 5.0 15 Betaine 3.0 3.0 3.0 3.0 16 Triethanolamine 1.0 1.0 1.0 1.0 17 Sodium hyaluronate 4.0 4.0 4.0 4.0 18 Distilled water Remaining amount Remaining amount Remaining amount Remaining amount 19 Preservative, fragrance, coloring a very small amount a very small amount a very small amount a very small amount Sum 100 100 100 100

Example 5: Experiment of Whitening Effect

The whitening effect was measured using the nutrition cream of Preparation Example prepared in Example 4 and the nutrition cream of Comparative Examples 1 to 3. Chromatame (Minolta CR300) was used for 10 healthy adult men and women with blemishes, freckles and pigmentation for 12 weeks. The change in brightness of color (ΔL) was measured.

The results of the experiment are shown in Table 4 below.

Subject Change in brightness of skin color (ΔL) Production Example Comparative Example 1 Comparative Example 2 Comparative Example 3 One 6.6 2.6 2.8 0.7 2 7.8 3.4 3.1 1.3 3 6.0 2.1 2.3 0.3 4 4.2 1.8 1.5 0.2 5 4.9 1.7 1.8 0.3 6 5.1 1.9 2.0 0.5 7 4.1 1.2 1.1 0.1 8 5.8 1.5 1.8 0.4 9 7.5 2.2 2.2 0.6 10 7.8 3.0 2.9 1.1 medium 5.98 2.14 2.15 0.55

As shown in Table 4, the nutritional cream of the preparation example in which the upper limb extract and niacinamide were simultaneously added, Comparative Example 1 in which only the upper limb extract was added, Comparative Example 2 in which only niacinamide was added, and the comparative example in which the two substances were not added at all. Compared to the nutritional cream of 3, the average value of ΔL was very high. Therefore, the cosmetic composition comprising the upper limb extract and niacinamide of the present invention has a very good skin whitening effect due to the synergistic action of two activities, the inhibitory effect of tyrosinase activity of the upper limb extract and the melanosomal migration inhibitory effect of niacinamide. It can be seen that.

Below, example Invention As an example of formulation softness toilet water, convergence toilet water, nutrition toilet water, massage cream, essence And Pack To illustrate However, example Invention Of cosmetic composition The formulation Therefore Restricted Is no.

Formulation Example 1 Flexible Lotion

ingredient Content (% by weight) Upper limb extract 5.0 Niacinamide 5.0 glycerin 5.0 1,3-butylene glycol 3.0 PEG 1500 1.0 Allantoin 0.1 DL-panthenol 0.3 EDTA-2Na 0.02 Benzophenone-9 0.04 Sodium hyaluronate 5.0 ethanol 10.0 Octicdodeceth-16 0.2 Polysorbate 20 0.2 Preservative, fragrance, coloring a very small amount Distilled water Remaining amount Sum 100

Formulation Example 2: Convergence Lotion

ingredient Content (% by weight) Upper limb extract 5.0 Niacinamide 5.0 glycerin 2.0 1,3-butylene glycol 2.0 Allantoin 0.2 DL-panthenol 0.2 EDTA-2Na 0.02 Benzophenone-9 0.04 Sodium hyaluronate 3.0 ethanol 15.0 Polysorbate 20 0.3 Witch hazel extract 2.0 Citric acid a very small amount Preservative, fragrance, coloring a very small amount Distilled water Remaining amount Sum 100

Formulation Example 3: Nutritional Lotion

ingredient Content (% by weight) Upper limb extract 5.0 Niacinamide 5.0 Glyceryl Stearate SE 1.5 Stearyl alcohol 1.5 lanolin 1.5 Polysorbate 1.3 Sorbitan stearate 0.5 Cured Vegetable Oil 1.0 Mineral oil 5.0 Squalane 3.0 Trioctanoine 2.0 Dimethicone 0.8 Tocopherol Acetate 0.5 Carboxyvinyl Polymer 0.12 glycerin 5.0 1,3-butylene glycol 3.0 Sodium hyaluronate 5.0 Triethanolamine 0.12 Preservative, fragrance, coloring a very small amount Distilled water Remaining amount Sum 100

Formulation Example 4: Massage Cream

ingredient Content (% by weight) Upper limb extract 5.0 Niacinamide 5.0 Lipophilic Monostearic Acid Glycerin 1.5 Stearyl alcohol 1.5 Stearic acid 1.0 Polysorbate 60 1.5 Sorbitan stearate 0.6 Isostearyl Isosterate 5.0 Squalane 5.0 Mineral oil 35.0 Dimethicone 0.5 Hydroxyethyl cellulose 0.12 glycerin 6.0 Triethanolamine 0.7 Preservative, fragrance, coloring a very small amount Distilled water Remaining amount Sum 100

Formulation Example 5: Essence

ingredient Content (% by weight) Upper limb extract 5.0 Niacinamide 5.0 glycerin 10.0 Betaine 5.0 PEG 1500 2.0 Allantoin 0.1 DL-panthenol 0.3 EDTA-2Na 0.02 Benzophenone-9 0.04 Hydroxyethyl cellulose 0.1 Sodium hyaluronate 8.0 Carboxyvinyl Polymer 0.2 Triethanolamine 0.18 Octyldodecanol 0.3 Octyldodeceth-16 0.4 ethanol 6.0 Preservative, fragrance, coloring a very small amount Distilled water Remaining amount Sum 100

Formulation Example 6: Pack

ingredient Content (% by weight) Upper limb extract 5.0 Niacinamide 5.0 Polyvinyl alcohol 15.0 Cellulose gum 0.15 glycerin 3.0 PEG 1500 2.0 Chicdestrin 0.15 DL-panthenol 0.4 Allantoin 0.1 Glycyrisin Monoammonium 0.3 Nicotinamide 0.5 ethanol 6.0 PEG 40 Cured Castor Oil 0.3 Preservative, fragrance, coloring a very small amount Distilled water Remaining amount Sum 100

As described above in detail a specific part of the present invention, it is apparent to those of ordinary skill in the art that such a specific technology is only a preferred embodiment, and the scope of the present invention is not limited thereto. Thus, the substantial scope of the present invention will be defined by the appended claims and equivalents thereof.

As described in detail above, the present invention provides a skin whitening cosmetic composition comprising the upper limb extract and niacinamide as an active ingredient. The cosmetic composition of the present invention is remarkably superior to the whitening cosmetic composition containing only the upper limb extract, which is a conventional whitening agent, due to the synergistic effect of tyrosinase activity inhibitory effect of the upper limb extract and melanoma transfer inhibition effect of niacinamide Skin whitening effect.

Claims (4)

A cosmetic composition for skin whitening comprising the extract of the upper limbs and niacinamide as an active ingredient. The cosmetic composition for skin whitening according to claim 1, wherein the content of the upper limb extract is 0.5-10.0 wt% based on the total weight of the composition. The cosmetic composition for skin whitening according to claim 1, wherein the content of niacinamide is 0.5-10.0 wt% based on the total weight of the composition. The group of claim 1 wherein the composition consists of a solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, surfactant-containing cleansing, oil, powder foundation, emulsion foundation, wax foundation and spray Cosmetic composition for skin whitening, characterized in that it has a formulation selected from.